Lamotrigina 100 mg 28 tab, Lamotrigina
INDICATIONS: Anticonvulsant, treatment of bipolar depression and mood stabilizer. (Lamotrigine) is a compound of the feniltriazinas, is a antiepilético used as monotherapy or as complementary to other antiepileptic drugs in partial seizures and / or generalized, including tonic-clonic seizures and seizures associated with Lennox-Gastaut syndrome.
(Lamotrigine) is also indicated for bipolar depression and mood stabilizer and has proven useful in the management of mania.
Not recommended for initial monotherapy in newly diagnosed pediatric patients. Once that has been achieved seizure control with combination therapy, concomitant antiepileptic drugs may be discontinued and the patient can continue with (lamotrigine) monotherapy.
requires less frequency of administration of the drug throughout the course of treatment, which ensures therapeutic compliance for their easy dosing, while achieving a reduction or elimination of local and systemic adverse effects. This is determined by eliminating the peaks (peaks) of the drug concentration.
Human Pharmacokinetics: Lamotrigine is a drug for the treatment of epilepsy. Is an antiepileptic derivative feniltriazina blocking repetitive activation induced sustained depolarization of neurons in the spinal cord in vitro action support blocking sodium channels, voltage-dependent, for this mechanism stabilizes neuronal membranes and inhibits presynaptic release of neurotransmitters, particularly glutamate. It is also a weak inhibitor of dihydrofolate reductase. It is fast and completely absorbed from the gastrointestinal tract, moderate binds to proteins (55%) and metabolized primarily in the liver by conjugation with glucuronic acid.
Brain and nerves are formed by a large number of nerve cells that communicate with each other through electrical impulses. These impulses must be regulated carefully between the brain and nerves for proper operation. When signals are in the form abnormally rapid and repetitive, the brain becomes overloaded, and its performance is affected. Lamotrigine prevents excessive accumulation, rapid and repetitive electrical impulses. Thus electrical nerve activity in the brain is stabilized, preventing seizures and maintaining brain activity. Lamotrigine inhibits tonic extension of the hind quarters in the model of maximal electroshock seizures.
Lamotrigine is absorbed rapidly and completely in the intestinal tract, with no significant effect of first pass metabolism. Peak plasma concentrations occur at about 2 to 5 hours after oral administration. The pharmacokinetics are linear up to 450 mg, which is the highest single dose tested. Plasma protein binding is 55% of which is unlikely to spread to lamotrigine of these toxic effects.
The clearance of lamotrigine is primarily metabolic with subsequent elimination of glucuronide conjugates in urine. Less than 10% is excreted as unchanged in the urine.
Its elimination half-life is 25 hours, which is modified substantially in the presence of other anticonvulsants. Only about 2% of the drug is excreted in the feces.
UDP-glucuronyltransferases have been identified as the enzyme responsible for metabolism of lamotrigine. This drug induce its own metabolism in a modest degree, depending on the dose. However, there is no evidence that lamotrigine affects the pharmacokinetics of other AEDs and data suggest that it is unlikely to present interactions between lamotrigine and drugs metabolised in the cytochrome P-450.
The half-life of lamotrigine is greatly affected by concomitant medication. When lamotrigine with enzyme-inducing drugs such as carbamazepine, phenytoin, phenobarbital or prednisone average half-life is reduced to about 14 hours and when coadministered with sodium valproate inhibits meatabolismo of lamotrigine, resulting in increased concentrations lamotrigine. The half-life of lamotrigine is generally shorter in children than in adults, with an average of 7 hours when administered with carbamazepine and phenytoin and increasing to 45-50 hours when co-administered with sodium valproate. The administration of lamotrigine in elderly patients, indicated that no dose adjustments required. In renal failure patients on lamotrigine pharmacokinetics is little affected, but plasma concentrations of the major metabolite glucuronide increased almost 8 times because of decreased renal clearance.
Pharmacological studies suggest that lamotrigine is a blocker, dependent on the use of sodium channels. Crash use-dependent and voltage sustained repetitive firing neurons and inhibits pathological release of glutamate (an amino acid that plays a key role in the generation of seizures), besides inhibiting the action potentials evoked by glutamate . Obtained with constant levels of active ingredient in blood reaching the desired effect, keeping it for an extended period. It also allows control of drug bioavailability.
CONTRAINDICATIONS: (lamotrigine) is contraindicated in cases of hypersensitivity to lamotrigine during pregnancy and lactation and in children under 2 years. Use with caution in cases of cardiac conduction disorders, liver or kidney dysfunction, thalassemia. Enzyme inducers (carbamazepine, phenobarbital, phenytoin, primidone) reduce the average life of lamotrigine. Valproic acid prolongs the shelf life. Alcohol and other CNS depressants increases its sedative.
PRECAUTIONS: Avoid handling dangerous machinery and vehicles during treatment. Avoid ingestion of alcohol or other central nervous system depressants. Do not discontinue treatment abruptly. Overdoses recommended at initiation of treatment may be associated with a high incidence of rash requiring discontinuation of treatment. Abrupt withdrawal of lamotrigine may provoke rebound seizures, so it is recommended that dose reduction in stages over a period of two weeks. Administered with caution to patients with renal disorders since there is an accumulation of metabolites of lamotrigine although its plasma concentration is similar to that detected in healthy patients. As this drug is metabolized primarily in the liver, is recom-mended to avoid its use in patients with liver diseases (cirrhosis, hepatitis).
There are reports of adverse skin reactions, which generally have occurred within the first eight weeks after initiation of treatment with lamotrigine. Most rashes are mild and self-limiting, however, have reported serious rashes that may endanger life and include: Stevens-Johnson syndrome and toxic epidermal necrolysis.
In children, the initial presentation of a rash can be mistaken for an infection, the physician should consider the possibility of a drug reaction in children with symptoms of rash and fever during the first eight weeks of treatment.
When patients develop rashes should be evaluated quickly and Lamotrigine should be discontinued immediately unless the rash is clearly not drug related.
Lamotrigine is a weak inhibitor of dihydrofolate reductase, in THEREFORE, the possibility of interference with folate metabolism during long term treatment. There are reports in the literature in relation to severe seizures including status epilepticus that may lead to rhabdomyolysis, multiple organ failure and Disseminated intravascular coagulation, sometimes with fatal results. There have been similar cases in association with the use of lamotrigine.
RESTRICTIONS OF USE DURING PREGNANCY AND BREASTFEEDING (lamotrigine) should not be used during pregnancy unless, in the opinion of the physician the potential benefits of treatment to the mother outweigh the possible risks to the product. Preliminary data indicate that lamotrigine passes into breast milk in concentrations of the order of 40-45% of plasma concentrations. In the small number of infants who received the drug known, it was estimated that the dose of lamotrigine was approximately 0.06 to 0.75 mg/kg/24 hours.
Side effects that should be reported to your doctor immediately: More common: rash.
Less common: increased seizures.
Rare: blistering, peeling of the skin, dark urine, fever, chills, or sore throat and flu symptoms, red or irritated eyes, itching, cramping, pain or weakness in the muscles, small red spots on the skin, sores, ulcers or white spots in mouth or on lips, swelling of the face, mouth, hands or feet, swollen glands, difficult breathing, unusual bleeding or bruising, unusual tiredness or weakness, yellow eyes or skin.
Signs of overdose: Clumsiness or unsteadiness (severe) coma, reciprocating or rotary movements continuous and uncontrolled eye (severe), dizziness (severe) sleep (severe), dry mouth, headache, increased Heart rate, babbling (severe).
Other side effects that should be reported to your doctor: More Common: blurred or double vision or any change in vision, clumsiness or unsteadiness: poor coordination.
Less common: anxiety, confusion, depression, irritability, or other mood or mental changes; reciprocating or rotary movements continuous and uncontrolled eye; infection.
Rare: memory loss.
Side effects that usually do not require medical attention: These side effects may go away during treatment, but if they continue or are bothersome, consult your doctor.
More common: dizziness (more common in women), sleep, headache, nausea, vomiting.
Less common: constipation, diarrhea, dry mouth, indigestion, loss of strength, menstrual pain, pain, runny nose, stammering, trembling or shaking, trouble sleeping, unusual weight loss.
DRUG INTERACTIONS AND OTHER GENDER: There is no evidence that lamotrigine affects clinically significant concentrations of hepatic oxidative enzymes. Lamotrigine may induce its own metabolism but the effect is modest and unlikely to have significant clinical consequences. Controlled studies have shown no evidence that lamotrigine affects the plasma concentrations of concomitant antiepileptic drugs tees. Evidence from in vitro studies indicates that lamotrigine does not displace other antiepileptic drug binding sites to proteins. In studies conducted in volunteers, lamotrigine did not affect plasma concentrations of ethinyl estradiol and levonorgestrel after administration of the contraceptive pill. However, and as with the introduction of another term therapy in patients receiving oral contraceptives, any change in menstrual bleeding pattern should be reported. Antiepileptic agents such as phenytoin, carbamazepine, phenobarbital and primidone, which induce liver enzymes that metabolize other drugs, increase the metabolism of lamotrigine. Valproate, reduces the metabolism of lamotrigine.
There have been reports of adverse events in the central nervous system such as dizziness, ataxia, diplopia, blurred vision and nausea in patients receiving carbamazepine following the introduction of lamotrigine. These events are usually reversible when dosage is reduced carbamazepine.
CHANGES IN RESULTS OF LABORATORY TESTS (lamotrigine) is a weak inhibitor of dihydrofolate reductase and, therefore, the possibility of interference with folate metabolism in long-term therapy. However, prolonged therapy studies, lamotrigine not induce significant changes in the concentration of hemoglobin.
PRECAUTIONS IN RELATION TO EFFECTS Carcinogenesis, Mutagenesis, Impairment of Fertility: In long-term studies conducted in rats and mice, there was no evidence of carcinogenicity using. In a wide range of mutagenicity assessments represent a genetic risk to man. Because Lamotrigine is a weak inhibitor of dihydrofolate reductase, there is a theoretical risk of fetal malformations in humans when the mother is treated with this enzyme inhibitors during pregnancy. However, in animal toxicology studies, reproductive stage-in higher than therapeutic doses in humans of lamotrigine, no teratogenic effects were observed.
LAMOTRIGINE administration did not affect fertility in reproduction studies in animals or humans.
DOSAGE AND ADMINISTRATION: Oral.
Dosage for treatment of epilepsy: The starting dose for adults as monotherapy is 25 mg once a day for two weeks, continuing with 50 mg once daily for the next two weeks, then increased to a maximum of 50 to 100 mg every 12 or 24 hours a week up to a usual maintenance dose of 100-200 mg a day every 12 or 24 hours.
Scaling the recommended dose for children 2 to 12 years of age for the treatment of epilepsy: In patients undergoing treatment of valproate with / without another antiepileptic drug first and the second week is recommended total daily dose of 0.15 mg / kg once a day, third and fourth week is recommended daily dose of 0.3 mg / kg, in increments of 0.3 mg / kg for 1 to 2 weeks to reach a maintenance dose of 1 to 5 mg / kg per day, either every 12 hours or every 24 hours to a maximum of 200 mg / day.
In patients receiving antiepileptic drugs that are inducers of enzymes, such as phenytoin, carbamazepine, phenobarbital and primidone, the first and second week should be considered a daily dose of 0.6 mg / kg every 12 hours, in the third and fourth week recommended dose is 1.2 mg / kg every 12 hours. The maintenance dose should be given in increments of 1.2 mg / kg body weight one to two weeks to reach a final dose of 5 mg / kg, divided into 2 doses up to 400 mg per day.
Scaling the recommended doses for over 12 years of age: The recommended maintenance dose is 100 mg to 400 mg every 12 or 24 hours.
In patients who are taking AEDs where the pharmacokinetic interaction with lamotrigine is unknown, the recommended dose escalation for lamotrigine with valproate is as follows: The first and second week 25 mg every other day, third and fourth week 25 mg once day, the fifth week 50 mg once every 12 or 24 hours.
The recommended maintenance dose of 100 mg every 24 hours or in two doses (every 12 hours).
Recommended treatment for adults over 18 years in treating bipolar disorder: If the patient is in a treatment regimen based prior valproate, the first and second week should begin with a treatment of 10 mg and 25 mg continue every third day. The third and fourth week should continue with 25 mg once daily.
And in the fifth week should continue Lamdra 50 mg with 24 SBK ® 50 mg every 24 hours or 12 Lamdra SBK ® 25 mg every 12 hours. The maintenance dose will end with Lamdra SBK 24 ® 100 mg every 24 hours.
Whether a drug treatment regimen enzyme inducers eg phenobarbital and carbamazepine, the first and second week with dose may start Lamdra SBK 24 ® 50 mg once daily, three week and four 12 ® from SBK Lamdra 100 mg in two divided doses per week five 200 mg in two divided doses.
The recommended maintenance dose is 300 mg administered every 24 hours and a week later, if necessary, increase the dose to 400 mg per day.
If the patient is treated with drugs known clinical interaction with lamotrigine, eg fluoxetine, venlafaxine, bupropion or lithium, or if you choose lamotrigine monotherapy, the first and second week is recommended Lamdra SBK 24 ® 25 mg every 24 hours, in the third and fourth week week recommended SBK 24 ® Lamdra of
50 mg every 24 hours, and in the fifth week is recommended Lamdra SBK 24 ® 100 mg once daily or in two divided doses (Lamdra SBK 12 ®).
The maintenance dose of the sixth to seventh week recommended dose of 100 mg to 400 mg as a single dose or divided into two doses.
MANIFESTATIONS AND MANAGEMENT OF OVERDOSE OR ACCIDENTAL INGESTION have been reported in a few cases, patients who received between 10 and 20 times the maximum therapeutic dose of lamotrigine. The clinical CONSEQUENCES were not severe, the signs and symptoms consisted of nystagmus, ataxia, dizziness, drowsiness, headache and vomiting.
In cases of overdose, the patient should be hospitalized and appropriate supportive treatment. If indicated, gastric lavage should be performed.
Drug Name: LAMOTRIGINE
Comparable drug patent: LAMICTAL
Active substance: LAMOTRIGINE
Extended-release tablets: No
Laboratory SOLARA, Inc. DE CV
Box of 28 Tablets
Made In: Mexico